专利号:US-2011319644-A1 优先权日:2006-11-02 标 题:Process for production of 1-hydroxy-19-norcyclovitamin d derivative and intermediate for the production 发明人:TOYODA ASAKO; NAGAI HAZUKI; KONUKI KANAME; TSUCHIDA TOSHIO 权利人:TOYODA ASAKO; NAGAI HAZUKI; KONUKI KANAME; TSUCHIDA TOSHIO 摘要:A cyclovitamin D derivative produced from 25-hydroxyvitamin D is reacted with osmium tetraoxide or a permanganic acid salt to produce a 10,19-diolcyclovitamin D derivative. The 10,19-diolcyclovitamin D derivative is reacted with a perhalogenic acid salt or lead tetraacetate to produce a 10-oxocyclovitamin D derivative. A 1-hydroxycyclovitamin D derivative is produced from the 10-oxocyclovitamin D derivative via a cyclovitamin D derivative and a 1,10-olefincyclovitamin D derivative. The 1-hydrocyclovitamin D derivative is subjected to solvolysis, thereby producing a 1-hydroxy-19-norviatmin D derivative. Thus provided are a novel process for production of 1-hydroxy-19-norcyclovitamin D derivative that is utilizable as an intermediate in the synthesis of 1-hydroxy-19-norvitamin D derivative which is useful as a pharmaceutical agent; and an intermediate for the production.
专利号:US-2022162188-A1 优先权日:2019-01-15 标 题:Isoprenoids and methods of making thereof 发明人:WILLIAMS GAVIN; LUND SEAN; HALL RACHAEL 权利人:UNIV NORTH CAROLINA STATE 摘要:Disclosed are methods for preparing isoprenoid subunits, as well as methods of employing these isoprenoid subunits for the synthesis of isoprenoids. Also provided are isoprenoids prepared using the methods described herein.
专利号:US-2005287169-A1 优先权日:2003-06-17 标 题 :Methods of use of genes of pyridoxal 5'-phosphate biosynthesis in Bacillus subtilis: avirulent strains for vaccines, and methods for identification of antibacterial agents 发明人:BELITSKY BORIS R 权利人:BELITSKY BORIS R 摘要:Methods and compositions comprising a pathogenic bacterial strain having a non-reverting mutation in a pdx gene encoding an enzyme involved in pyridoxal-5′-phosphate synthesis are provided, for use in vaccines, and methods for identification of inhibitors of the enzyme for use as an antibacterial agent are provided.
专利号:EP-1608751-B1 优先权日:2003-03-28 标题 :Method for the in vivo modification of the synthesis activity of a metabolite by means of the modification of a gene the activity of which is not the original activity 发明人:KAMINSKI PIERRE-ALEXANDRE; MARLIERE PHILIPPE 权利人:PASTEUR INSTITUT; CENTRE NAT RECH SCIENT 摘要:The invention relates to a method for altering a protein X such as to modify the characteristics thereof by a) obtaining the mutants X* of the sequence coding for protein X, by means of aleatory mutagenesis, b) transformation of cells with a phenotype [P-] with vectors comprising the mutated nucleic acids obtained in step (a) which code for proteins X*, where P- signifies that said cells are auxotrophic for substance P, P begin the product of the action of X on the natural substrate thereof S, c) culturing said cells in a medium comprising a substrate S*, S* being an analogue of the natural substrate S of the protein X, d) selection of the cells [P-:: X*] which have survived step c) in which the proteins X* can biosynthesise the product P from the substrate S*. The invention further relates to mutated proteins X, nucleic acids, expression vectors, host cells comprising a vector, use of N-dideoxyribosyl transferases for the transfer of a dideoxyribose (ddR) from a dideoxyribonucleoside to another nucleoside, a method for production of compounds comprising a step using a mutated protein and a strain of E. coli .
专利号:US-7892838-B2 优先权日:2003-03-28 标题 :Method for the in vivo modification of the synthesis activity of a metabolite by means of the modification of a gene the activity of which is not the original activity 发明人:KAMINSKI PIERRE-ALEXANDRE; MARLIERE PHILIPPE 权利人:PASTEUR INSTITUT; CENTRE NAT RECH SCIENT 摘要:The invention relates to a method for altering a protein X such as to modify the characteristics thereof by a) obtaining the mutants X* of the sequence coding for protein X, by means of aleatory mutagenesis, b) transformation of cells with a phenotype [P-] with vectors comprising the mutated nucleic acids obtained in step (a) which code for proteins X*, where P-signifies that said cells are auxotrophic for substance P, P begin the product of the action of X on the natural substrate thereof S, c) culturing said cells in a medium comprising a substrate S*, S* being an analogue of the natural substrate S of the protein X, d) selection of the cells [P-:: X*] which have survived step c) in which the proteins X* can biosynthesise the product P from the substrate S*. The invention further relates to mutated proteins X, nucleic acids, expression vectors, host cells comprising a vector, use of N-dideoxyribosyl transferases for the transfer of a dideoxyribose (ddR) from a dideoxyribonucleoside to another nucleoside, a method for production of compounds comprising a step using a mutated protein and a strain of E. coli.
专利号:US-6936600-B2 优先权日:1999-04-01 标题:Sorbitol dehrydrogenase inhibitors 发明人:CHU-MOYER MARGARET Y; MYLARI BANAVARA L; ZEMBROWSKI WILLIAM J 权利人:PFIZER 摘要:This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, n n nwherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.